Strategies for Targeting PI3K Proliferate

Strategies for Targeting PI3K Proliferate

Other early efforts focused on dual inhibitors of PI3K (pan–class I) and its downstream target mTOR; these drugs largely suffered a fate similar to that of pan–class I inhibitors.17 Several continue to be evaluated in clinical trials, however; notable among them is the oral PI3K/mTOR inhibitor paxalisib (GDC0084). Most current clinical trials of this agent, which penetrates the blood-brain barrier, are in brain cancer; PI3K pathway upregulation has been demonstrated in 85% of glioblastoma cases.18,19

Paxalisib is being evaluated in patients with newly diagnosed glioblastoma and unmethylated MGMT promoter status in an ongoing phase 2 trial (NCT03522298). Results of an interim analysis showed a median PFS of 8.4 months and overall survival of 17.5 months among 24 patients treated at the maximum-tolerated dose of 60 mg. The most common toxicities were rash, stomatitis, hyperglycemia, fatigue, nausea, and decreased appetite.19

https://www.onclive.com/view/strategies-for-targeting-pi3k-proliferate

IMO our chances of approval are extremely high, given the number of FDA approvals granted for the various PI3K class of drugs discussed in this article,

Regards..